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EA201200095A1 - PHARMACEUTICAL COMPOSITIONS AND SOLID FORMS - Google Patents

PHARMACEUTICAL COMPOSITIONS AND SOLID FORMS

Info

Publication number
EA201200095A1
EA201200095A1 EA201200095A EA201200095A EA201200095A1 EA 201200095 A1 EA201200095 A1 EA 201200095A1 EA 201200095 A EA201200095 A EA 201200095A EA 201200095 A EA201200095 A EA 201200095A EA 201200095 A1 EA201200095 A1 EA 201200095A1
Authority
EA
Eurasian Patent Office
Prior art keywords
hydroxymethylpyrimidin
trifluoromethylphenyl
yloxy
naphthalene
amide
Prior art date
Application number
EA201200095A
Other languages
Russian (ru)
Inventor
Йёрг Бергхаузен
Клэр Ог
Михаэль Хербиг
Бинь Сюй
Стефани Жона
Раджендер Лелети
Йозеф Готтфрид Майнгасснер
Стефани Монье
Маттиас Напп
Махавир Прашад
Антон Штютц
Ранджит Тхакур
Original Assignee
Новартис Аг
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Новартис Аг filed Critical Новартис Аг
Publication of EA201200095A1 publication Critical patent/EA201200095A1/en

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
    • A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
    • A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/10—Dispersions; Emulsions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/04—Antipruritics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/34—One oxygen atom

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Dermatology (AREA)
  • Virology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Cardiology (AREA)
  • Biotechnology (AREA)
  • Pain & Pain Management (AREA)
  • Molecular Biology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Dispersion Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicinal Preparation (AREA)

Abstract

В заявке описаны фармацевтические композиции, включающие (3-трифторметилфенил)амид 6-((6-гидроксиметилпиримидин-4-илокси)нафталин-1-карбоновой кислоты), применение (3-трифторметилфенил)амида 6-((6-гидроксиметилпиримидин-4-илокси)нафталин-1-карбоновой кислоты) и композиций, включающих (3-трифторметилфенил)амид 6-((6-гидроксиметилпиримидин-4-илокси)нафталин-1-карбоновой кислоты), при лечении, прежде всего показаний, связанных с дисрегуляцией/сверхэкспрессией VEFG, (нео)васкуляризацией и VEGF-опосредованным ангиогенезом, а также способы получения указанных композиций, в заявке кроме того описаны конкретные формы (3-трифторметилфенил)амида 6-((6-гидроксиметилпиримидин-4-илокси)нафталин-1-карбоновой кислоты), а также получение и применение указанных форм. В заявке также описан новый способ получения (3-трифторметилфенил)амида 6-((6-гидроксиметилпиримидин-4-илокси)нафталин-1-карбоновой кислоты).The application describes pharmaceutical compositions comprising 6 - ((6-hydroxymethylpyrimidin-4-yloxy) naphthalene-1-carboxylic acid (3-trifluoromethylphenyl) amide), the use of 6 - ((6-hydroxymethylpyrimidin-4- (3-trifluoromethylphenyl) amide) yloxy) naphthalene-1-carboxylic acid) and compositions comprising (3-trifluoromethylphenyl) amide 6 - ((6-hydroxymethylpyrimidin-4-yloxy) naphthalene-1-carboxylic acid), in the treatment of, first of all, indications associated with dysregulation / overexpression of VEFG, (neo) vascularization and VEGF-mediated angiogenesis, as well as methods for obtaining a decree of these compositions, the application furthermore describes specific forms of (3-trifluoromethylphenyl) amide 6 - ((6-hydroxymethylpyrimidin-4-yloxy) naphthalene-1-carboxylic acid), as well as the preparation and use of these forms. The application also describes a new process for the preparation of (3-trifluoromethylphenyl) amide 6 - ((6-hydroxymethylpyrimidin-4-yloxy) naphthalene-1-carboxylic acid).

EA201200095A 2009-07-06 2010-07-05 PHARMACEUTICAL COMPOSITIONS AND SOLID FORMS EA201200095A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US22326909P 2009-07-06 2009-07-06
PCT/EP2010/059553 WO2011003858A2 (en) 2009-07-06 2010-07-05 Pharmaceutical compositions and solid forms

Publications (1)

Publication Number Publication Date
EA201200095A1 true EA201200095A1 (en) 2012-08-30

Family

ID=42686504

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201200095A EA201200095A1 (en) 2009-07-06 2010-07-05 PHARMACEUTICAL COMPOSITIONS AND SOLID FORMS

Country Status (20)

Country Link
US (1) US20110112121A1 (en)
EP (1) EP2451458A2 (en)
JP (1) JP2012532183A (en)
KR (1) KR20120041745A (en)
CN (1) CN102470134A (en)
AR (1) AR077549A1 (en)
AU (1) AU2010270361A1 (en)
BR (1) BR112012000383A2 (en)
CA (1) CA2767440A1 (en)
CO (1) CO6480987A2 (en)
EA (1) EA201200095A1 (en)
EC (1) ECSP12011578A (en)
IL (1) IL217329A0 (en)
MA (1) MA33417B1 (en)
MX (1) MX2012000391A (en)
SG (1) SG176955A1 (en)
TN (1) TN2011000653A1 (en)
TW (1) TW201113258A (en)
WO (1) WO2011003858A2 (en)
ZA (1) ZA201200079B (en)

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NZ583284A (en) 2007-08-17 2012-04-27 Novartis Ag Cyclic depsipeptides from isolated chondromyces crocatus useful as inhibitors of kallikrein 7 and human neutrophil elastase
AR086168A1 (en) 2011-04-20 2013-11-27 Novartis Ag PROCESSES FOR THE ELABORATION OF MACROCICLICAL AND INTERMEDIARY DEPSIPEPTIDES
US8680054B2 (en) * 2011-04-20 2014-03-25 Novartis Ag Suspension type topical formulations comprising cyclic depsipeptide
US8987413B2 (en) 2012-10-09 2015-03-24 Novartis Ag Aldehyde acetal based processes for the manufacture of macrocyclic depsipeptides and new intermediates
US9067978B2 (en) 2012-10-09 2015-06-30 Novartis Ag Solution phase processes for the manufacture of macrocyclic depsipeptides and new intermediates
CN104860885B (en) 2014-02-24 2017-11-17 中国科学院上海药物研究所 Naphthoyl aminated compounds, preparation method and use
SE1751461A1 (en) * 2017-11-28 2019-05-29 Ascilion Ab Method of detecting an exogenous agent in interstitial fluid
WO2019126270A1 (en) * 2017-12-20 2019-06-27 Sienna Biopharmaceuticals, Inc. Formulations for dermal delivery of polymer conjugates of indolocarbazole compounds with reduced exposure
WO2026006488A1 (en) * 2024-06-26 2026-01-02 Antinous Technology Company Limited Angiogenesis inhibitors and uses thereof

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WO2008031835A2 (en) * 2006-09-13 2008-03-20 Novartis Ag Method of treating autoimmune diseases using vegf-pathway inhibitors

Also Published As

Publication number Publication date
CA2767440A1 (en) 2011-01-13
WO2011003858A2 (en) 2011-01-13
BR112012000383A2 (en) 2016-03-29
US20110112121A1 (en) 2011-05-12
MA33417B1 (en) 2012-07-03
CN102470134A (en) 2012-05-23
IL217329A0 (en) 2012-02-29
AU2010270361A1 (en) 2012-01-19
MX2012000391A (en) 2012-02-28
TN2011000653A1 (en) 2013-05-24
SG176955A1 (en) 2012-01-30
ZA201200079B (en) 2012-09-26
CO6480987A2 (en) 2012-07-16
KR20120041745A (en) 2012-05-02
EP2451458A2 (en) 2012-05-16
WO2011003858A3 (en) 2011-03-03
ECSP12011578A (en) 2012-02-29
TW201113258A (en) 2011-04-16
JP2012532183A (en) 2012-12-13
AR077549A1 (en) 2011-09-07

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